Drug intelligence / Profile preview

erlotinib + satraplatin

Development stage
Unknown
Lead developer
GPC Biotech
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib + satraplatin is a combination therapy consisting of erlotinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and satraplatin, an oral platinum analog chemotherapeutic agent. This combination has been investigated for potential synergistic effects in cancer treatment. Preclinical studies showed that JM118 (the active metabolite of satraplatin) sensitivity was enhanced most significantly when JM118 preceded erlotinib administration, which was associated with increased formation of DNA-platinum adducts. The combination increased G2/M phase accumulation and enhanced apoptosis. The mechanism of synergy involved a combination of effects on platinum-DNA adduct formation, cell cycle distribution, and signaling pathways. The combination has been studied particularly for non-small cell lung cancer (NSCLC) in elderly patients who may not be candidates for aggressive combination systemic chemotherapy.

Brand names
Tarceva + satraplatin
Other names
satraplatin + erlotinib
02

Targets

ABCG2 (Breast cancer resistance protein)ABCB1 (P-glycoprotein)EGFR (Epidermal growth factor receptor)DNA

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